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Inhibition of serotonin transport by (+)McN5652 is noncompetitive.

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Inhibition of serotonin transport by (+)McN5652 is noncompetitive. / Hummerich, René; Schulze, Oliver; Rädler, Thomas; Mikecz, Pal; Reimold, Matthias; Brenner, Winfried; Clausen, Malte; Schloss, Patrick; Buchert, Ralph.

In: NUCL MED BIOL, Vol. 33, No. 3, 3, 2006, p. 317-323.

Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review

Harvard

Hummerich, R, Schulze, O, Rädler, T, Mikecz, P, Reimold, M, Brenner, W, Clausen, M, Schloss, P & Buchert, R 2006, 'Inhibition of serotonin transport by (+)McN5652 is noncompetitive.', NUCL MED BIOL, vol. 33, no. 3, 3, pp. 317-323. <http://www.ncbi.nlm.nih.gov/pubmed/16631080?dopt=Citation>

APA

Hummerich, R., Schulze, O., Rädler, T., Mikecz, P., Reimold, M., Brenner, W., Clausen, M., Schloss, P., & Buchert, R. (2006). Inhibition of serotonin transport by (+)McN5652 is noncompetitive. NUCL MED BIOL, 33(3), 317-323. [3]. http://www.ncbi.nlm.nih.gov/pubmed/16631080?dopt=Citation

Vancouver

Hummerich R, Schulze O, Rädler T, Mikecz P, Reimold M, Brenner W et al. Inhibition of serotonin transport by (+)McN5652 is noncompetitive. NUCL MED BIOL. 2006;33(3):317-323. 3.

Bibtex

@article{d72c0ea6063b4d528c69dbd4bbd290e3,
title = "Inhibition of serotonin transport by (+)McN5652 is noncompetitive.",
abstract = "INTRODUCTION: Imaging of the serotonergic innervation of the brain using positron emission tomography (PET) with the serotonin transporter (SERT) ligand [11C] (+)McN5652 might be affected by serotonin in the synaptic cleft if there is relevant interaction between [11C] (+)McN5652 and serotonin at the SERT. The aim of the present study therefore was to pharmacologically characterize the interaction of [11C] (+)McN5652 and serotonin at the SERT. METHODS: In vitro saturation analyses of [3H]serotonin uptake into HEK293 cells stably expressing the human SERT were performed in the absence and presence of unlabelled (+)McN5652. Data were evaluated assuming Michaelis-Menten kinetics. RESULTS: Unlabelled (+)McN5652 significantly reduced the maximal rate of serotonin transport V(max) of SERT without affecting the Michaelis-Menten constant K(M). CONCLUSIONS: This finding indicates that (+)McN5652 inhibits serotonin transport through the SERT in a noncompetitive manner. This might suggest that [11C] (+)McN5652 PET is not significantly affected by endogenous serotonin.",
author = "Ren{\'e} Hummerich and Oliver Schulze and Thomas R{\"a}dler and Pal Mikecz and Matthias Reimold and Winfried Brenner and Malte Clausen and Patrick Schloss and Ralph Buchert",
year = "2006",
language = "Deutsch",
volume = "33",
pages = "317--323",
journal = "NUCL MED BIOL",
issn = "0969-8051",
publisher = "Elsevier Inc.",
number = "3",

}

RIS

TY - JOUR

T1 - Inhibition of serotonin transport by (+)McN5652 is noncompetitive.

AU - Hummerich, René

AU - Schulze, Oliver

AU - Rädler, Thomas

AU - Mikecz, Pal

AU - Reimold, Matthias

AU - Brenner, Winfried

AU - Clausen, Malte

AU - Schloss, Patrick

AU - Buchert, Ralph

PY - 2006

Y1 - 2006

N2 - INTRODUCTION: Imaging of the serotonergic innervation of the brain using positron emission tomography (PET) with the serotonin transporter (SERT) ligand [11C] (+)McN5652 might be affected by serotonin in the synaptic cleft if there is relevant interaction between [11C] (+)McN5652 and serotonin at the SERT. The aim of the present study therefore was to pharmacologically characterize the interaction of [11C] (+)McN5652 and serotonin at the SERT. METHODS: In vitro saturation analyses of [3H]serotonin uptake into HEK293 cells stably expressing the human SERT were performed in the absence and presence of unlabelled (+)McN5652. Data were evaluated assuming Michaelis-Menten kinetics. RESULTS: Unlabelled (+)McN5652 significantly reduced the maximal rate of serotonin transport V(max) of SERT without affecting the Michaelis-Menten constant K(M). CONCLUSIONS: This finding indicates that (+)McN5652 inhibits serotonin transport through the SERT in a noncompetitive manner. This might suggest that [11C] (+)McN5652 PET is not significantly affected by endogenous serotonin.

AB - INTRODUCTION: Imaging of the serotonergic innervation of the brain using positron emission tomography (PET) with the serotonin transporter (SERT) ligand [11C] (+)McN5652 might be affected by serotonin in the synaptic cleft if there is relevant interaction between [11C] (+)McN5652 and serotonin at the SERT. The aim of the present study therefore was to pharmacologically characterize the interaction of [11C] (+)McN5652 and serotonin at the SERT. METHODS: In vitro saturation analyses of [3H]serotonin uptake into HEK293 cells stably expressing the human SERT were performed in the absence and presence of unlabelled (+)McN5652. Data were evaluated assuming Michaelis-Menten kinetics. RESULTS: Unlabelled (+)McN5652 significantly reduced the maximal rate of serotonin transport V(max) of SERT without affecting the Michaelis-Menten constant K(M). CONCLUSIONS: This finding indicates that (+)McN5652 inhibits serotonin transport through the SERT in a noncompetitive manner. This might suggest that [11C] (+)McN5652 PET is not significantly affected by endogenous serotonin.

M3 - SCORING: Zeitschriftenaufsatz

VL - 33

SP - 317

EP - 323

JO - NUCL MED BIOL

JF - NUCL MED BIOL

SN - 0969-8051

IS - 3

M1 - 3

ER -